BIBP3226 inhibits neuropeptide Y and pancreatic polypeptide potentiated neurogenic vasoconstriction
Neuropeptide Y (NPY) potentiates the contractile response of the rat caudal artery to adrenergic nerve stimulation in-vitro. The NPY Y 1 selective antagonist BIBP3226 ((R)-N 2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-argininamide), inhibited the vascular effects of NPY in rat caudal artery prepa...
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| Veröffentlicht in: | Life sciences (1973) 1998, Vol.62 (6), p.525-532 |
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| container_title | Life sciences (1973) |
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| creator | Barrios, Victor E. Nelson, Allyson G. Toombs, Christopher F. |
| description | Neuropeptide Y (NPY) potentiates the contractile response of the rat caudal artery to adrenergic nerve stimulation
in-vitro. The NPY Y
1 selective antagonist BIBP3226 ((R)-N
2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-argininamide), inhibited the vascular effects of NPY in rat caudal artery preparations
in-vitro (IC
50 = 126 nM). BIBP3226 also inhibited the effects of the selective Y
1 agonist [Leu
31,Pro
34]NPY and completely abolished the effects of avian pancreatic polypeptide that was shown to be capable of potentiating neurogenic vasoconstriction in this preparation. These effects were reversible and are most likely mediated by the Y
1 receptor subtype since we failed to observe any functional evidence of a Y
2 receptor subtype in rat caudal artery. The caudal artery provides a useful functional assay for pharmacological analysis of NPY and NPY antagonists. |
| doi_str_mv | 10.1016/S0024-3205(97)01148-X |
| format | Article |
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in-vitro. The NPY Y
1 selective antagonist BIBP3226 ((R)-N
2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-argininamide), inhibited the vascular effects of NPY in rat caudal artery preparations
in-vitro (IC
50 = 126 nM). BIBP3226 also inhibited the effects of the selective Y
1 agonist [Leu
31,Pro
34]NPY and completely abolished the effects of avian pancreatic polypeptide that was shown to be capable of potentiating neurogenic vasoconstriction in this preparation. These effects were reversible and are most likely mediated by the Y
1 receptor subtype since we failed to observe any functional evidence of a Y
2 receptor subtype in rat caudal artery. The caudal artery provides a useful functional assay for pharmacological analysis of NPY and NPY antagonists.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/S0024-3205(97)01148-X</identifier><identifier>PMID: 9464464</identifier><language>eng</language><publisher>Netherlands: Elsevier Inc</publisher><subject>Animals ; Arginine - analogs & derivatives ; Arginine - pharmacology ; avian pancreatic polypeptide ; BIBP3226 ; In Vitro Techniques ; Leu 31 ; Male ; neurogenic vasoconstriction ; neuropeptide Y ; Neuropeptide Y - antagonists & inhibitors ; Pancreatic Polypeptide - antagonists & inhibitors ; Pro 34]NPY ; Rats ; Rats, Sprague-Dawley ; Receptors, Neuropeptide Y - antagonists & inhibitors ; Sympathetic Nervous System - physiology ; Vasoconstriction - drug effects</subject><ispartof>Life sciences (1973), 1998, Vol.62 (6), p.525-532</ispartof><rights>1998</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c391t-7364841e8de856447ccb27a5284e9efbf343178a4db864416e3173c13d850a693</citedby><cites>FETCH-LOGICAL-c391t-7364841e8de856447ccb27a5284e9efbf343178a4db864416e3173c13d850a693</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0024-3205(97)01148-X$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,4021,27921,27922,27923,45993</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9464464$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Barrios, Victor E.</creatorcontrib><creatorcontrib>Nelson, Allyson G.</creatorcontrib><creatorcontrib>Toombs, Christopher F.</creatorcontrib><title>BIBP3226 inhibits neuropeptide Y and pancreatic polypeptide potentiated neurogenic vasoconstriction</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>Neuropeptide Y (NPY) potentiates the contractile response of the rat caudal artery to adrenergic nerve stimulation
in-vitro. The NPY Y
1 selective antagonist BIBP3226 ((R)-N
2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-argininamide), inhibited the vascular effects of NPY in rat caudal artery preparations
in-vitro (IC
50 = 126 nM). BIBP3226 also inhibited the effects of the selective Y
1 agonist [Leu
31,Pro
34]NPY and completely abolished the effects of avian pancreatic polypeptide that was shown to be capable of potentiating neurogenic vasoconstriction in this preparation. These effects were reversible and are most likely mediated by the Y
1 receptor subtype since we failed to observe any functional evidence of a Y
2 receptor subtype in rat caudal artery. The caudal artery provides a useful functional assay for pharmacological analysis of NPY and NPY antagonists.</description><subject>Animals</subject><subject>Arginine - analogs & derivatives</subject><subject>Arginine - pharmacology</subject><subject>avian pancreatic polypeptide</subject><subject>BIBP3226</subject><subject>In Vitro Techniques</subject><subject>Leu 31</subject><subject>Male</subject><subject>neurogenic vasoconstriction</subject><subject>neuropeptide Y</subject><subject>Neuropeptide Y - antagonists & inhibitors</subject><subject>Pancreatic Polypeptide - antagonists & inhibitors</subject><subject>Pro 34]NPY</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, Neuropeptide Y - antagonists & inhibitors</subject><subject>Sympathetic Nervous System - physiology</subject><subject>Vasoconstriction - drug effects</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc1KJDEUhYM4aNv6CEKtRBc1k1RS-VmJijpCwwyMgq5CKrmtke6kTNKCb2-0e9wKgRDOd3Iv5yB0SPBPggn_9Q_jjrW0w_2xEieYECbb-y00IVKoFnNKttHkC9lFezk_Y4z7XtAdtKMYZ_VMkD2_Of9Lu443Pjz5wZfcBFilOMJYvIPmoTHBNaMJNoEp3jZjXLz9F8dYIBRvCri16xFCRV5NjjaGXJK3xcewj37MzSLDweaeorury9uL3-3sz_XNxdmstVSR0grKmWQEpAPZ1_WEtUMnTN9JBgrmw5wySoQ0zA2yyoRDfVJLqJM9NlzRKTpa_zum-LKCXPTSZwuLhQkQV1kLxSXpifwWJJxyhRWvYL8GbYo5J5jrMfmlSW-aYP3Rgv5sQX9ErJXQny3o--o73AxYDUtwX65N7FU_XetQ43j1kHS2HoIF5xPYol3030x4BzNbl2Y</recordid><startdate>1998</startdate><enddate>1998</enddate><creator>Barrios, Victor E.</creator><creator>Nelson, Allyson G.</creator><creator>Toombs, Christopher F.</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7TK</scope><scope>7X8</scope></search><sort><creationdate>1998</creationdate><title>BIBP3226 inhibits neuropeptide Y and pancreatic polypeptide potentiated neurogenic vasoconstriction</title><author>Barrios, Victor E. ; Nelson, Allyson G. ; Toombs, Christopher F.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c391t-7364841e8de856447ccb27a5284e9efbf343178a4db864416e3173c13d850a693</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Animals</topic><topic>Arginine - analogs & derivatives</topic><topic>Arginine - pharmacology</topic><topic>avian pancreatic polypeptide</topic><topic>BIBP3226</topic><topic>In Vitro Techniques</topic><topic>Leu 31</topic><topic>Male</topic><topic>neurogenic vasoconstriction</topic><topic>neuropeptide Y</topic><topic>Neuropeptide Y - antagonists & inhibitors</topic><topic>Pancreatic Polypeptide - antagonists & inhibitors</topic><topic>Pro 34]NPY</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, Neuropeptide Y - antagonists & inhibitors</topic><topic>Sympathetic Nervous System - physiology</topic><topic>Vasoconstriction - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Barrios, Victor E.</creatorcontrib><creatorcontrib>Nelson, Allyson G.</creatorcontrib><creatorcontrib>Toombs, Christopher F.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Barrios, Victor E.</au><au>Nelson, Allyson G.</au><au>Toombs, Christopher F.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>BIBP3226 inhibits neuropeptide Y and pancreatic polypeptide potentiated neurogenic vasoconstriction</atitle><jtitle>Life sciences (1973)</jtitle><addtitle>Life Sci</addtitle><date>1998</date><risdate>1998</risdate><volume>62</volume><issue>6</issue><spage>525</spage><epage>532</epage><pages>525-532</pages><issn>0024-3205</issn><eissn>1879-0631</eissn><abstract>Neuropeptide Y (NPY) potentiates the contractile response of the rat caudal artery to adrenergic nerve stimulation
in-vitro. The NPY Y
1 selective antagonist BIBP3226 ((R)-N
2-(diphenylacetyl)-N-[(4-hydroxyphenyl)methyl]-argininamide), inhibited the vascular effects of NPY in rat caudal artery preparations
in-vitro (IC
50 = 126 nM). BIBP3226 also inhibited the effects of the selective Y
1 agonist [Leu
31,Pro
34]NPY and completely abolished the effects of avian pancreatic polypeptide that was shown to be capable of potentiating neurogenic vasoconstriction in this preparation. These effects were reversible and are most likely mediated by the Y
1 receptor subtype since we failed to observe any functional evidence of a Y
2 receptor subtype in rat caudal artery. The caudal artery provides a useful functional assay for pharmacological analysis of NPY and NPY antagonists.</abstract><cop>Netherlands</cop><pub>Elsevier Inc</pub><pmid>9464464</pmid><doi>10.1016/S0024-3205(97)01148-X</doi><tpages>8</tpages></addata></record> |
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| ispartof | Life sciences (1973), 1998, Vol.62 (6), p.525-532 |
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| language | eng |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Animals Arginine - analogs & derivatives Arginine - pharmacology avian pancreatic polypeptide BIBP3226 In Vitro Techniques Leu 31 Male neurogenic vasoconstriction neuropeptide Y Neuropeptide Y - antagonists & inhibitors Pancreatic Polypeptide - antagonists & inhibitors Pro 34]NPY Rats Rats, Sprague-Dawley Receptors, Neuropeptide Y - antagonists & inhibitors Sympathetic Nervous System - physiology Vasoconstriction - drug effects |
| title | BIBP3226 inhibits neuropeptide Y and pancreatic polypeptide potentiated neurogenic vasoconstriction |
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